Brexpiprazole (BioDeep_00000858533)
代谢物信息卡片
化学式: C25H27N3O2S (433.18238820000005)
中文名称: 溴苯哌唑
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: C1CN(CCN1CCCCOC2=CC3=C(C=C2)C=CC(=O)N3)C4=C5C=CSC5=CC=C4
InChI: InChI=1S/C25H27N3O2S/c29-25-9-7-19-6-8-20(18-22(19)26-25)30-16-2-1-11-27-12-14-28(15-13-27)23-4-3-5-24-21(23)10-17-31-24/h3-10,17-18H,1-2,11-16H2,(H,26,29)
描述信息
D018377 - Neurotransmitter Agents > D015259 - Dopamine Agents > D018491 - Dopamine Agonists
C78272 - Agent Affecting Nervous System > C29710 - Antipsychotic Agent
N - Nervous system > N05 - Psycholeptics > N05A - Antipsychotics
D018377 - Neurotransmitter Agents > D018490 - Serotonin Agents
Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[1][2].
同义名列表
2 个代谢物同义名
数据库引用编号
7 个数据库交叉引用编号
- ChEBI: CHEBI:134716
- KEGGdrug: D10309
- PubChem: 11978813
- DrugBank: DB09128
- ChEMBL: CHEMBL2105760
- CAS: 913611-97-9
- medchemexpress: HY-15780
分类词条
相关代谢途径
Reactome(0)
BioCyc(0)
PlantCyc(0)
代谢反应
0 个相关的代谢反应过程信息。
Reactome(0)
BioCyc(0)
WikiPathways(0)
Plant Reactome(0)
INOH(0)
PlantCyc(0)
COVID-19 Disease Map(0)
PathBank(0)
PharmGKB(0)
0 个相关的物种来源信息
在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有：
- PubMed: 来源于PubMed文献库中的文献信息，我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表，这个列表按照代谢物同时出现的文献数量降序排序，取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
- NCBI Taxonomy: 通过文献数据挖掘，得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序，取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
- Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
- Chemical Reaction: 在化学反应过程中，存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。
点击图上的相关代谢物的名称，可以跳转到相关代谢物的信息页面。
文献列表
- Kouji Fukuyama, Eishi Motomura, Motohiro Okada. Brexpiprazole Reduces 5-HT7 Receptor Function on Astroglial Transmission Systems.
International journal of molecular sciences.
2022 Jun; 23(12):. doi:
10.3390/ijms23126571. [PMID: 35743014] - Peter Manu. Repurposing Drugs for Post-COVID-19 Fatigue Syndrome: Methylphenidate, Duloxetine, and Brexpiprazole.
American journal of therapeutics.
2022 01; 29(2):e229-e230. doi:
10.1097/mjt.0000000000001471. [PMID: 35389574] - Ahmed Elmokadem, Christopher D Bruno, Conrad Housand, Eric Burroughs Jordie, Christina R Chow, Lawrence J Lesko, David J Greenblatt. Brexpiprazole Pharmacokinetics in CYP2D6 Poor Metabolizers: Using Physiologically Based Pharmacokinetic Modeling to Optimize Time to Effective Concentrations.
Journal of clinical pharmacology.
2022 01; 62(1):66-75. doi:
10.1002/jcph.1946. [PMID: 34328221] - Christopher D Bruno, Ahmed Elmokadem, Conrad Housand, Eric Burroughs Jordie, Christina R Chow, Thomas P Laughren, David J Greenblatt. Impact of Obesity on Brexpiprazole Pharmacokinetics: Proposal for Improved Initiation of Treatment.
Journal of clinical pharmacology.
2022 01; 62(1):55-65. doi:
10.1002/jcph.1947. [PMID: 34339048] - De-Juan Li, Qin Yue, Lu Liu, Ke-Ke Che, Xue-Mei Liu, Chang-Hua Hu. Brexpiprazole caused glycolipid metabolic disorder by inhibiting GLP1/GLP1R signaling in rats.
Acta pharmacologica Sinica.
2021 Aug; 42(8):1267-1279. doi:
10.1038/s41401-021-00680-x. [PMID: 33976388] - Bangqing Wu, Lijun Wu, Yingju He, Zongning Yin, Li Deng. Engineered PLGA microspheres for extended release of brexpiprazole: in vitro and in vivo studies.
Drug development and industrial pharmacy.
2021 Jun; 47(6):1001-1010. doi:
10.1080/03639045.2021.1934859. [PMID: 34032181] - Kouji Fukuyama, Motohiro Okada. Effects of Atypical Antipsychotics, Clozapine, Quetiapine and Brexpiprazole on Astroglial Transmission Associated with Connexin43.
International journal of molecular sciences.
2021 May; 22(11):. doi:
10.3390/ijms22115623. [PMID: 34070699] - Dean F Wong, Arash Raoufinia, Patricia Bricmont, James R Brašić, Robert D McQuade, Robert A Forbes, Tetsuro Kikuchi, Hiroto Kuwabara. An open-label, positron emission tomography study of the striatal D2/D3 receptor occupancy and pharmacokinetics of single-dose oral brexpiprazole in healthy participants.
European journal of clinical pharmacology.
2021 May; 77(5):717-725. doi:
10.1007/s00228-020-03021-9. [PMID: 33196868] - Sheng Feng, Jeffrey R Enders, Oneka T Cummings, Erin C Strickland, Timothy McIntire, Gregory McIntire. A Dilute and Shoot LC-MS/MS Method for Antipsychotics in Urine.
Journal of analytical toxicology.
2020 May; 44(4):331-338. doi:
10.1093/jat/bkz098. [PMID: 31776574] - Congcong Yu, Liuliu Pan, Guangbao Wang, Ziyao Cai, Yancan Zhou, Xuyong Zheng, Ce Chen, Xiaodan Zhang. Silybin enhances the blood concentration of brexpiprazole in rats by downregulating expression of CYP3A4 and CYP2D6.
Die Pharmazie.
2020 05; 75(5):198-200. doi:
10.1691/ph.2020.9935. [PMID: 32393428] - Ragy R Girgis, Andy Forbes, Anissa Abi-Dargham, Mark Slifstein. A positron emission tomography occupancy study of brexpiprazole at dopamine D2 and D3 and serotonin 5-HT1A and 5-HT2A receptors, and serotonin reuptake transporters in subjects with schizophrenia.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology.
2020 04; 45(5):786-792. doi:
10.1038/s41386-019-0590-6. [PMID: 31847007] - Disha Thakkar, Abhijeet S Kate. In silico, in vitro and in vivo metabolite identification of brexpiprazole using ultra-high-performance liquid chromatography/quadrupole time-of-flight mass spectrometry.
Rapid communications in mass spectrometry : RCM.
2019 May; 33(11):1024-1035. doi:
10.1002/rcm.8436. [PMID: 30889624] - Molly A Kwiatkowski, Gerhard Hellemann, Catherine A Sugar, Zackary A Cope, Arpi Minassian, William Perry, Mark A Geyer, Jared W Young. Dopamine transporter knockdown mice in the behavioral pattern monitor: A robust, reproducible model for mania-relevant behaviors.
Pharmacology, biochemistry, and behavior.
2019 03; 178(?):42-50. doi:
10.1016/j.pbb.2017.12.007. [PMID: 29289701] - Qiaogen Zou, Ran Yan, Wei Liu, Ping Wei. A Validated Quantification Method for Brexpiprazole in Dog Plasma.
Journal of chromatographic science.
2018 Sep; 56(8):702-708. doi:
10.1093/chromsci/bmy045. [PMID: 29800104] - Jun Ishigooka, Shuichi Iwashita, Koushi Higashi, Ei Leen Liew, Yoshihiro Tadori. Pharmacokinetics and Safety of Brexpiprazole Following Multiple-Dose Administration to Japanese Patients With Schizophrenia.
Journal of clinical pharmacology.
2018 Jan; 58(1):74-80. doi:
10.1002/jcph.979. [PMID: 28750151] - Morgane Milienne-Petiot, Mark A Geyer, Jørn Arnt, Jared W Young. Brexpiprazole reduces hyperactivity, impulsivity, and risk-preference behavior in mice with dopamine transporter knockdown-a model of mania.
Psychopharmacology.
2017 Mar; 234(6):1017-1028. doi:
10.1007/s00213-017-4543-7. [PMID: 28160035] - John M Kane, Aleksandar Skuban, Mary Hobart, John Ouyang, Emmanuelle Weiller, Catherine Weiss, Christoph U Correll. Overview of short- and long-term tolerability and safety of brexpiprazole in patients with schizophrenia.
Schizophrenia research.
2016 07; 174(1-3):93-98. doi:
10.1016/j.schres.2016.04.013. [PMID: 27188270] - Christoph U Correll, Aleksandar Skuban, John Ouyang, Mary Hobart, Stephanie Pfister, Robert D McQuade, Margaretta Nyilas, William H Carson, Raymond Sanchez, Hans Eriksson. Efficacy and Safety of Brexpiprazole for the Treatment of Acute Schizophrenia: A 6-Week Randomized, Double-Blind, Placebo-Controlled Trial.
The American journal of psychiatry.
2015 Sep; 172(9):870-80. doi:
10.1176/appi.ajp.2015.14101275. [PMID: 25882325]